Tapentadol Hydrochloride

Tschentke, T.M.; Vry, Jean De; Terlinden, Rolf; Hennies, Hagen‐Heinrich; Lange, Claudia; Strassburger, W.; Haurand, Michael; Kolb, J.; Schneider, Johannes; Buschmann, Helmut; Finkam, M.; Jahnel, Ulrich; Friedrichs, E.

doi:10.1358/dof.2006.031.12.1047744

Cited by 124 publications

(104 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Thus, the supraspinal analgesia of tapentadol seems driven mainly by MOR, and supraspinal tapentadol is clearly less potent compared with supraspinal morphine. Similar data on both drugs reported for rodent models of acute somatic and visceral nociception after systemic and intracerebroventricular administration (Tzschentke et al, 2006) are in line with this finding. As with the supraspinal route, spinal administration resulted in similar efficacy for tapentadol and morphine.…”

Section: Discussionsupporting

confidence: 89%

Spinal-Supraspinal and Intrinsicµ-Opioid Receptor Agonist-Norepinephrine Reuptake Inhibitor (MOR-NRI) Synergy of Tapentadol in Diabetic Heat Hyperalgesia in Mice

Christoph

Schröder

Tallarida

et al. 2013

J Pharmacol Exp Ther

View full text Add to dashboard Cite

Tapentadol is a m-opioid receptor (MOR) agonist and norepinephrine reuptake inhibitor (NRI) with established efficacy in neuropathic pain in patients and intrinsic synergistic interaction of both mechanisms as demonstrated in rodents. In diabetic mice, we analyzed the central antihyperalgesic activity, the occurrence of site-site interaction, as well as the spinal contribution of opioid and noradrenergic mechanisms in a hotplate test. Tapentadol (0.1-3.16 mg/animal) showed full efficacy after intrathecal as well as after intracerebroventricular administration (ED 50 0.42 mg/animal i.t., 0.18 mg/animal i.c.v.). Combined administration of equianalgesic doses revealed spinal-supraspinal synergy (ED 50 0.053 mg/animal i.t. 1 i.c.v.). Morphine (0.001-10 mg/animal) also showed central efficacy and synergy (ED 50 0.547 mg/animal i.t., 0.004 mg/animal i.c.v., 0.014 mg/animal i.t. 1 i.c.v.). Supraspinal potencies of tapentadol and morphine correlated with the 50-fold difference in their MOR affinities. In contrast, spinal potencies of both drugs were similar and correlated with their relative systemic potencies (ED 50 0.27 mg/kg i.p. tapentadol, 1.1 mg/kg i.p. morphine). Spinal administration of the opioid antagonist naloxone or the a 2 -adrenoceptor antagonist yohimbine before systemic administration of equianalgesic doses of tapentadol (1 mg/kg i.p.) or morphine (3.16 mg/kg i.p.) revealed pronounced influence on opioidergic and noradrenergic pathways for both compounds. Tapentadol was more sensitive toward both antagonists than was morphine, with median effective dose values of 0.75 and 1.72 ng/animal i.t. naloxone and 1.56 and 2.04 ng/animal i.t. yohimbine, respectively. It is suggested that the antihyperalgesic action of systemically administered tapentadol is based on opioid spinal-supraspinal synergy, as well as intrinsic spinally mediated MOR-NRI synergy.

show abstract

Section: Discussionsupporting

confidence: 89%

Spinal-Supraspinal and Intrinsicµ-Opioid Receptor Agonist-Norepinephrine Reuptake Inhibitor (MOR-NRI) Synergy of Tapentadol in Diabetic Heat Hyperalgesia in Mice

Christoph

Schröder

Tallarida

et al. 2013

J Pharmacol Exp Ther

View full text Add to dashboard Cite

show abstract

“…It occurs in the context of many diseases and conditions, including cancer, back pain, osteoarthritis, trauma, fibromyalgia, diabetic neuropathy, post-operative pain, and migraine-related headache. A recent market research report indicates that more than 1.5 billion people worldwide suffer from chronic pain and that approximately 3-4.5% of the global population suffers from neuropathic pain (1).…”

Section: Introductionmentioning

confidence: 99%

“…Conventional drug delivery systems have little control over the drug release and so effective concentration at the 1 TIFAC CORE in NDDS, Pharmacy Department, Faculty of Technology & Engineering, The M.S. University of Baroda, Kalabhavan, Vadodara, 390 001, India.…”

Section: Introductionmentioning

confidence: 99%

Development and Evaluation of a Once-Daily Controlled Porosity Osmotic Pump of Tapentadol Hydrochloride

2015

View full text Add to dashboard Cite

Abstract. The present study aimed to prepare, optimize, and evaluate Tapentadol hydrochloride controlled porosity osmotic pump (CPOP) and to achieve the drug release at nearly zero-order. The CPOP was prepared by the coating of polymers (Eudragit RSPO and RLPO) on a directly compressed core tablet. A Box-behnken experimental design was applied to optimize the parameters for CPOP. The optimized batch was characterized for in vitro drug release study, effect of pH, osmolarity and agitation intensity, and surface morphology and stability study. In vivo pharmacokinetic studies were performed on New Zealand white rabbits for CPOP and marketed tablet. All the batches showed a drug release ranging from 29.87 to 56.92% after 12 h; and from 59.64 to 99.96% after 24 h. There was no change in the drug release pattern at different pH and agitation intensities. The drug release was found to decrease with increasing osmolarity of dissolution media.An in vivo study showed a higher mean residence time, area under the curve, and biological half-life (T 1/2 ) than the marketed tablet with low rate of elimination (Ke) and a 2.35-fold increase in relative bioavailability. The result showed that the amounts of sodium chloride and PEG 400 were contributing positively while the number of coats was negatively affecting the drug release. The drug release was found to be independent of physiological conditions. The stability testing showed that the prepared CPOP was stable for 3 months at accelerated conditions. The prepared CPOP was found to deliver Tapentadol hydrochloride at zero-order for up to 24 h.

show abstract

“…5,6 It is 14 times more efficacious than Tramadol and two times less to morphine. 21,22 Tapentadol immediate release tablets have been approved by the FDA in 2008 for the relief of moderate to severe acute pain in adults and in 2011, for chronic pain in an extended release form. 23 In all 4 phase 3 studies of Tapentadol for acute pain, improvements in pain intensity were observed with Tapentadol treatment (50 mg every 4 to 6 hours).…”

Section: Discussionmentioning

confidence: 99%

A comparative study of oral tapentadol with thoracic epidural analgesia versus intravenous tramadol and paracetamol combination for postoperative analgesia in off pump CABG

Shah

Jaishree

Bhavsar

2013

Int J Basic Clin Pharmacol

View full text Add to dashboard Cite

Tapentadol Hydrochloride

Cited by 124 publications

References 0 publications

Spinal-Supraspinal and Intrinsicµ-Opioid Receptor Agonist-Norepinephrine Reuptake Inhibitor (MOR-NRI) Synergy of Tapentadol in Diabetic Heat Hyperalgesia in Mice

Spinal-Supraspinal and Intrinsicµ-Opioid Receptor Agonist-Norepinephrine Reuptake Inhibitor (MOR-NRI) Synergy of Tapentadol in Diabetic Heat Hyperalgesia in Mice

Development and Evaluation of a Once-Daily Controlled Porosity Osmotic Pump of Tapentadol Hydrochloride

A comparative study of oral tapentadol with thoracic epidural analgesia versus intravenous tramadol and paracetamol combination for postoperative analgesia in off pump CABG

Contact Info

Product

Resources

About